autotaxin-in-3

Autotaxin-IN-3 是 Autotaxin 的抑制剂(IC50 = 2.4 nM)，Autotaxin 负责增加腹水和血浆中的溶血磷脂酸。

Lysophosphatidylcholine 18:2是一种小鼠代谢物，在功能上与亚油酸有关。1-亚油酰-2-羟基-SN-甘油-3-卵磷脂是氧化低密度脂蛋白的主要成分，​​​血浆中低水平的18:2 LysoPC与糖耐量受损、胰岛素抵抗、2 型糖尿病和冠状动脉疾病等代谢紊乱相关。1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC同时也是Autotaxin(LysoPLD)生成溶血磷脂酸(LPA)的底物，在细胞运动中起重要作用。

Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) 作为一种autotaxin (ATX) 抑制剂，具有中等效力，IC50值为620 nM。该化合物适用于黑色素瘤的研究。

Cyclic Phosphatidic Acids (cPAs) are naturally occurring lysophosphatidic acid (LPA) analogs, characterized by a 5-membered ring formed between the sn-2 hydroxy group and the sn-3 phosphate. Carba-derivatives of cPA (ccPA) modify the sn-2 (2-ccPA) or sn-3 (3-ccPA) linkage, hindering the conversion of cPA into LPA. Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) incorporates the 18:1 fatty acid oleate at the sn-1 position on the glycerol backbone, acting as a cyclic LPA analog. This compound, at a concentration of 25 μM, blocks MM1 cells' transcellular migration through mesothelial cell monolayers induced by fetal bovine serum (by 90.1%) or LPA (by 99.9%), without impeding cell proliferation. Additionally, 3-ccPA 18:1, in the 0.1-1.0 μM range, notably suppresses autotaxin, which plays a vital role in various cancer cell behaviors including survival, growth, migration, invasion, and metastasis.